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Purity: ≥98%
GK921 is a novel and potent inhibitor of transglutaminase 2 (TGase), with an IC50 of 7.71 μM for TGase 2 that is recombinant. GK921 was cytotoxic to RCC, with an average GI50 of 0.905 μM across eight RCC cell lines. In the preclinical xenograft tumor models ACHN and CAKI-1, a single treatment with GK921 stabilized p53 and nearly eliminated tumor growth. The TGase 2 inhibitor GK921 inhibits the growth of RCC in xenograft tumor models, indicating a potential novel therapeutic strategy for RCC.
| Targets |
TGase (IC50 = 7.71 μM)
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|---|---|
| ln Vitro |
GK921 inhibits the dose-dependent polymerization of p53 and I-κBα induced by TGase 2. GK921 was cytotoxic, with GI50 values ranging from 10-10 to 10-4 M. GI50 on average is 9.05×10-7 M. A concentration-dependent rise in cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels is seen when GK921 rescues p53 levels, which in turn triggers apoptosis[1].
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| ln Vivo |
GK921 stabilizes p53 in the preclinical xenograft tumor models ACHN and CAKI-1, almost completely reducing tumor growth after a single treatment[1].
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| Enzyme Assay |
Following a 10-minute preincubation period in 0.1 mL of reaction buffer containing varying concentrations of GK13 or GK921, with or without 10 mM CaCl2, TGase 2from guinea pig liver is added. The substrate solution contains 2
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| Cell Assay |
The BAX promoter luciferase reporter construct is transfected into the cells. The dual luciferase assay kit is used to measure the activities of firefly and Renilla luciferase after exposure to GK921 (0, 0.5, 1, 2.5, and 5 μM), with pRL-CMV serving as an internal control.
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| Animal Protocol |
Mice: GK921 is dissolved in DMSO for mice. For 64 days, the vehicle alone and GK921 (8 mg/kg) are given orally once daily, five days a week. Every two to three days, the size of the main tumors is measured with calipers. One calculates the tumor volume[1].
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| References |
| Molecular Formula |
C21H20N4O
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|---|---|
| Molecular Weight |
344.41
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| Exact Mass |
344.16
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| Elemental Analysis |
C, 73.23; H, 5.85; N, 16.27; O, 4.65
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| CAS # |
1025015-40-0
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| Related CAS # |
1025015-40-0
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| Appearance |
Solid powder
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| SMILES |
C1CCN(C1)CCOC2=NC3=C(N=CC=C3)N=C2C#CC4=CC=CC=C4
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| InChi Key |
MNYJJHBAEYKXEG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H20N4O/c1-2-7-17(8-3-1)10-11-19-21(26-16-15-25-13-4-5-14-25)24-18-9-6-12-22-20(18)23-19/h1-3,6-9,12H,4-5,13-16H2
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| Chemical Name |
3-(2-phenylethynyl)-2-(2-pyrrolidin-1-ylethoxy)pyrido[2,3-b]pyrazine
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| Synonyms |
GK921; GK-921; GK 921
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 30 mg/mL (~87.1 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.26 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9035 mL | 14.5176 mL | 29.0352 mL | |
| 5 mM | 0.5807 mL | 2.9035 mL | 5.8070 mL | |
| 10 mM | 0.2904 mL | 1.4518 mL | 2.9035 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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